Almorexant, also known as 2(R)-(6,7-dimethoxy-1(S)-(2-(4-(trifluoromethyl)phenyl)ethyl)-1,2,3,4-tetrahydroisoquinolin-2-yl)-N-methyl-2-phenylacetamide, acts as a dual OX-1/OX-2 receptor antagonist. The neuropeptide hormones, orexin-1 and orexin-2 (OX-1, OX-2), also known as orexin A and B, or hypocretin-1 and -2, are produced in the hypothalamus and play an important role in the sleep-wake cycle. Blockade of OX-1 and OX-2 receptors has been shown to induce somnolence. (Brisbare-Roch, C. et al., Nat. Med., February 2007, 13(2):150).
Almorexant is currently undergoing clinical trials for the treatment of insomnia.
Despite the beneficial activities of almorexant, there is a continuing need for new compounds to treat insomnia.